SGC0946

Name: SGC0946
Brand: MedChemExpress
SKU: HY-15650
Rating: 5.0 (12 reviews)

Cat. No.: HY-15650 Purity: 99.68%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

SGC0946 is a selective DOT1L inhibitor with an IC₅₀ value of 0.3 nM. By inhibiting DOT1L, SGC0946 can induce G1 phase arrest, suppress cell self-renewal and metastatic potential, and induce cell differentiation in cancer cells. SGC0946 can be used in the research of tumors such as leukemia and breast cancer, and also serves as a probe to further investigate the cellular mechanisms of DOT1L in normal and diseased cells.

For research use only. We do not sell to patients.

CAS No. : 1561178-17-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of SGC0946:

SGC0946 TFA Get quote

12 Publications Citing Use of MCE SGC0946

RT-PCR

Flow Cytometry

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

Cell Imaging/Staining

: SGC0946 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]; CCK-8 assay data showing the sensitivity of NCI-H460-DOT1L-WT/R231Q cells to SGC0946 (0.01,.0.1, 1, 10, 100 μM, 6 days).

: SGC0946 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]; CDX-bearing mice were treated with vehicle Cisplatin (3 mg/kg, twice per week), Vinorelbine (4 mg/kg, twice per week), or SGC0946 (20 mg/kg, five times per week) through intraperitoneal administration. The graphs show the tumor images and weights, with the tumor inhibition rate.

: SGC0946 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]; Crystal violet staining of NCI-H460-DOT1L-WT/R231Q cells treated with SGC0946 (2.5 or 7.5 μM), binimetinib (2.5 or 7.5 μM), or the combination at the same concentrations for 7 to 14 days (top). Comparison of relative colony formation between groups at 7.5 μM drug concentration.

: SGC0946 purchased from MedChemExpress. Usage Cited in: Elife. 2020 Oct 1;9:e57858. [Abstract]; Q-PCR analysis of the HOXA9^P2A-mCherry cells with or without the 6-day treatment of the DOT1L inhibitor SGC0946 by using specific primers targeting the mRNA sequences of mCherry and HOXA9. The correlation of transcription reduction in mCherry and HOXA9 in response to inhibitor–mediated transcription repression was calculated by performing Pearson’s correlation test.

: SGC0946 purchased from MedChemExpress. Usage Cited in: Elife. 2020 Oct 1;9:e57858. [Abstract]; Flow cytometry analysis of the HOXA9^P2A-mCherry cells treated with DMSO and various dosages of the DOT1L inhibitor SGC0946 (1, 5 μM).

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

DOT1L

0.3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	2.65 nM Compound: SGC0946	Downregulation of H3K79 methylation in human A-431 cells incubated for 3 to 4 days by microscopy based analysis Downregulation of H3K79 methylation in human A-431 cells incubated for 3 to 4 days by microscopy based analysis	[PMID: 23250418]
MCF-10A	IC₅₀	8.8 nM Compound: 37	Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level	[PMID: 25406853]
MCF-10A	IC₅₀	8.8 nM Compound: SGC0946	Downregulation of H3K79 methylation in human MCF-10A cells by fluorescence microscopy analysis Downregulation of H3K79 methylation in human MCF-10A cells by fluorescence microscopy analysis	[PMID: 23250418]
NCI-H460	IC₅₀	36.01 μM Compound: SGC0946	Antiproliferative activity against human NCI-H460 cells harboring DOT1L R231Q mutant (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H460 cells harboring DOT1L R231Q mutant (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 39255403]
NCI-H460	IC₅₀	8.83 μM Compound: SGC0946	Antiproliferative activity against human NCI-H460 cells harboring wildtype DOT1L (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H460 cells harboring wildtype DOT1L (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 39255403]

In Vitro

SGC0946 (0-100 μM; 4 days) inhibits DOT1L with IC₅₀ of 2.65 nM in A431 cells^[1].
SGC0946 (1, 5 μM; 14 days) displays selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells (transformed with the MLL-AF9 fusion oncogene)^[1].
SGC0946 (1 μM; 3-7 days) shows time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation^[1].
SGC0946 (1 μM, 7 days) effectively inhibits MLL target genes, HOXA9 and Meis1^[1].
SGC0946 (0.2, 2, or 20 μM; 12 days) reduces proliferation and survival of ovarian cancer cells by inhibiting DOT1L enzymatic activity^[2].
SGC0946 (10 μM; 12 days) induces G1 phase arrest by blocking DOT1L in SK-OV-3 and TOV21G cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	A431 cells
Concentration:	0-100 µM
Incubation Time:	4 days
Result:	Showed potent inhibitory activity against DOT1L with IC₅₀ of 2.65 nM in A431 cells.

Cell Viability Assay^[1]

Cell Line:	Human cord blood cells (transformed with the MLL-AF9 fusion oncogene).
Concentration:	1, 5 µM
Incubation Time:	14 days
Result:	Killed human cord blood cells transformed with an MLL-AF9 fusion oncogene.

Western Blot Analysis^[1]

Cell Line:	Molm13 MLL cells
Concentration:	1 µM
Incubation Time:	3-7 days
Result:	Reduced H3K79me2 in Molm13 MLL cells in a time- and dose-dependent manner, and a complete inhibition exhibited at day 7.

Cell Proliferation Assay^[2]

Cell Line:	SK-OV-3 and TOV21G cells
Concentration:	0.2, 2, or 20 μM
Incubation Time:	12 days
Result:	Inhibited the growth of both SK-OV-3 and TOV21G cells in a dose- and time-dependent manner. Reduced the colony of both SK-OV-3 and TOV21G cells.

Cell Cycle Analysis^[2]

Cell Line:	SK-OV-3 and TOV21G cells
Concentration:	10 μM
Incubation Time:	12 days
Result:	Induced increased G1 population and decreased S phase and G2/M phase cells in asynchronized SK-OV-3 and TOV21G cells.

In Vivo

SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female NOD-SCID mice (4-week-old; mouse orthotopic xenograft ovarian cancer model)^[2].
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; twice a week for 6 weeks.
Result:	Significantly suppressed growth of tumor (size and weight of tumor masses smaller than the untreated group). Inhibited DOT1L enzymatic activity and decreased H3K79me2,CDK6, and cyclin D3 levels in the tumors.

Molecular Weight

618.57

Formula

C₂₈H₄₀BrN₇O₄

CAS No.

1561178-17-3

Appearance

Solid

Color

White to yellow

SMILES

CC(C)(C1=CC=C(C=C1)NC(NCCCN(C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C4=C(C(Br)=C3)C(N)=NC=N4)O2)C(C)C)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (80.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6166 mL	8.0832 mL	16.1663 mL
5 mM	0.3233 mL	1.6166 mL	3.2333 mL
10 mM	0.1617 mL	0.8083 mL	1.6166 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.68%

Select Batch:

Data Sheet (279 KB) SDS (419 KB)

COA (248 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[1]. Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. [Content Brief]

[2]. Zhang X, et al. Prognostic and therapeutic value of disruptor of telomeric silencing-1-like (DOT1L) expression in patients with ovarian cancer. J Hematol Oncol. 2017 Jan 23;10(1):29. [Content Brief]

[3]. Zhang L, et al. Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancer. Oncotarget. 2014 Nov 15;5(21):10665-77. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6166 mL	8.0832 mL	16.1663 mL	40.4158 mL
	5 mM	0.3233 mL	1.6166 mL	3.2333 mL	8.0832 mL
	10 mM	0.1617 mL	0.8083 mL	1.6166 mL	4.0416 mL
	15 mM	0.1078 mL	0.5389 mL	1.0778 mL	2.6944 mL
	20 mM	0.0808 mL	0.4042 mL	0.8083 mL	2.0208 mL
	25 mM	0.0647 mL	0.3233 mL	0.6467 mL	1.6166 mL
	30 mM	0.0539 mL	0.2694 mL	0.5389 mL	1.3472 mL
	40 mM	0.0404 mL	0.2021 mL	0.4042 mL	1.0104 mL
	50 mM	0.0323 mL	0.1617 mL	0.3233 mL	0.8083 mL
	60 mM	0.0269 mL	0.1347 mL	0.2694 mL	0.6736 mL
	80 mM	0.0202 mL	0.1010 mL	0.2021 mL	0.5052 mL

SGC0946 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SGC09461561178-17-3SGC 0946SGC-0946Histone MethyltransferaseleukemiaMLL-rearrangeovarian cancerMolm13 MLLcord blood cellsSK-OV-3TOV21GInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

SGC0946

Customer Review

Other Forms of SGC0946:

SGC0946 Related Antibodies

12 Publications Citing Use of MCE SGC0946

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

SGC0946 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

SGC0946 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report